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首页> 外文期刊>RSC Advances >Design and synthesis of novel carbazolo-thiazoles as potential anti-mycobacterial agents using a molecular hybridization approach
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Design and synthesis of novel carbazolo-thiazoles as potential anti-mycobacterial agents using a molecular hybridization approach

机译：使用分子杂交方法设计和合成新型咔唑-噻唑类作为潜在抗分枝杆菌药

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Various substituted carbazolo-thiazoles (compounds 6a-6o) were synthesized in good yields using a molecular hybridization approach. The synthesized compounds were evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H(37)Rv strain at the National Institute of Allergy and Infectious Diseases (Bethesda, MD, USA). Among the tested series, compound 6c (minimum inhibitory concentration 21 mu M) showed the most promising anti-mycobacterial activity. Brief structure-activity relationship studies showed that the electron-donating groups (OCH3 and OH), particularly on the phenyl ring of the thiazole motif, had a positive correlation with the anti-mycobacterial activity. In addition, they displayed low cytotoxicity against a mammalian Vero cell line using the MTT assay, thereby having a high therapeutic index. This study shows the importance of molecular hybridization and the scope for the development of carbazole-thiazole compounds as potential anti-mycobacterial agents.
机译：使用分子杂交方法以高收率合成了各种取代的咔唑-噻唑（化合物6a-6o）。在美国过敏和传染病研究所（美国贝塞斯达，美国）评估了合成的化合物对结核分枝杆菌H（37）Rv菌株的体外抗结核活性。在测试系列中，化合物6c（最低抑制浓度为21μM）显示出最有希望的抗分枝杆菌活性。简短的结构-活性关系研究表明，给电子基团（OCH3和OH），尤其是噻唑基序的苯环上，与抗分枝杆菌活性呈正相关。另外，使用MTT测定法，它们显示出对哺乳动物Vero细胞系的低细胞毒性，从而具有高治疗指数。这项研究表明了分子杂交的重要性以及咔唑-噻唑化合物作为潜在抗分枝杆菌药物的开发范围。

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